| Reaction Details |
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 | Report a problem with these data |
| Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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| Ligand | BDBM50585940 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2164341 (CHEMBL5049202) |
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| IC50 | 70±n/a nM |
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| Citation |  Poddutoori, R; Aardalen, K; Aithal, K; Barahagar, SS; Belliappa, C; Bock, M; Chelur, S; Gerken, A; Gopinath, S; Gruenenfelder, B; Kiffe, M; Krishnaswami, M; Langowski, J; Madapa, S; Narayanan, K; Pandit, C; Panigrahi, SK; Perrone, M; Potakamuri, RK; Ramachandra, M; Ramanathan, A; Ramos, R; Sager, E; Samajdar, S; Subramanya, HS; Thimmasandra, DS; Venetsanakos, E; Möbitz, H Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action. J Med Chem65:4350-4366 (2022) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Dual specificity mitogen-activated protein kinase kinase 1 |
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| Name: | Dual specificity mitogen-activated protein kinase kinase 1 |
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| Synonyms: | Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAP2K1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | MEK1 | MP2K1_HUMAN | Mitogen-activated protein kinase 1 (MEK1) | PRKMK1 | VHL-MAP2K1/MAP2K2 |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 43439.03 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates. |
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| Residue: | 393 |
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| Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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| BDBM50585940 |
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| n/a |
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| Name | BDBM50585940 |
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| Synonyms: | CHEMBL5090765 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H22ClFN6O |
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| Mol. Mass. | 512.965 |
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| SMILES | Fc1cc2ncc3ncn(C4CCN(CC#N)CC4)c3c2cc1-c1ccc(Oc2ccccn2)cc1Cl |
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| Structure | 
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